Ritlecitinib

Ritlecitinib (PF-06651600) is a highly selective, orally active, irreversible covalent JAK3 inhibitor (IC50=33 nM) without inhibitory activity towards JAK1, JAK2, and TYK2 (IC50 >10 μ M) . Ritlecitinib rapidly inactivates the JAK3 kinase, and blocks signaling and downstream STAT phosphorylation mediated by common gamma chain cytokines such as IL-2 and IL-15. Ritlecitinib can inhibit Th1/Th17 cell differentiation and function, and effectively suppress preclinical animal models such as alopecia areata, adjuvant-induced arthritis (AIA), and experimental autoimmune encephalomyelitis (EAE) [1][2][3].

Product Specifications

CAS Number

[1792180-81-4]

Product Name Alternative

PF-06651600

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Interleukin Related; JAK; STAT

Type

Reference compound

Related Pathways

Epigenetics; Immunology/Inflammation; JAK/STAT Signaling; Protein Tyrosine Kinase/RTK; Stem Cell/Wnt

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/PF-06651600.html

Purity

99.80

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

C=CC(N1[C@@H](C)CC[C@@H](NC2=C3C(NC=C3)=NC=N2)C1)=O

Molecular Formula

C15H19N5O

Molecular Weight

285.35

Precautions

H302, H315, H319, H335

References & Citations

[1]Thorarensen A, et al. Design of a Janus Kinase 3 (JAK3) Specific Inhibitor 1- ((2 S, 5 R) -5- ((7 H-Pyrrolo [2, 3-d] pyrimidin-4-yl) amino) -2-methylpiperidin-1-yl) prop-2-en-1-one (PF-06651600) Allowing for the Interrogation of JAK3 Signaling in Humans. Journal of medicinal chemistry, 2017, 60 (5) : 1971-1993.|[2]Telliez JB, et al. Discovery of a JAK3-Selective Inhibitor: Functional Differentiation of JAK3-Selective Inhibition over pan-JAK or JAK1-Selective Inhibition. ACS Chem Biol. 2016 Dec 16;11 (12) :3442-3451.